Researching anti-tuberculosis agents

Dr. Tlabo Leboho is a researcher at the University of Limpopo in South Africa, working on the discovery and development of anti-tuberculosis agents.

Dr. Leboho’s research group recently published a paper in the ‘Bioorganic & Medicinal Chemistry Letters’ journal entitled: ‘Synthesis of novel quinoxaline-alkynyl derivatives and their anti-Mycobacterium tuberculosis activity.’

Back Row (L-R): Jackson K Nkoana, Terrinne P Mokoena, Tebogo MC Ragedi. Middle Row (L-R): Lebogang F Mabatamela, Dareos M Rakgoale, Mitchelle M Tukakgomo, Lerato A Raphoko. Front Row (L-R): Winston Nxumalo, Redolf S Segodi, Rosinah M Sedibana, Khomotso J Mokganya,  David T Rokhotso, Tlabo C Leboho.

Back Row (L-R): Jackson K Nkoana, Terrinne P Mokoena, Tebogo MC Ragedi. Middle Row (L-R): Lebogang F Mabatamela, Dareos M Rakgoale, Mitchelle M Tukakgomo, Lerato A Raphoko. Front Row (L-R): Winston Nxumalo, Redolf S Segodi, Rosinah M Sedibana, Khomotso J Mokganya, David T Rokhotso, Tlabo C Leboho. Image Credit: Asynt

Tuberculosis (TB) remains a serious health issue in South Africa and around the world, with as many as 1.4 million deaths from the disease in 2019.

The University of Limpopo began working on the critical field of anti-tuberculosis agents in 2013. Since joining the team around five years ago, Dr. Leboho has been collaborating with Winston Nxumalo, who joined the university around eight years ago.

Throughout this research, global health authorities have reported growing cases of multi-drug resistant TB (MDR-TB) and drug-resistant TB (XDR-TD).

The prevalence of these diseases creates significant problems for organizations seeking to treat and manage TB due to their need for longer treatment times and their lack of response to currently available drugs.

High incidences of MDR-TB and XDR-TB are more common in developing and low-income countries.

Researching-Anti-tuberculosis-Agents

Image Credit: Asynt

An interdisciplinary approach to drug development research and medicinal chemistry

Collaborations with other departments and specialists are vital to Dr. Leboho’s work because chemists are often unable to perform many of the biological assays required to evaluate the efficacy of the synthesized compounds amounting from the research.

Biologists have the skillset and available tools to determine synthesized compounds’ toxicity, activity, bioavailability and other pharmacological properties.

The research described in here details the synthesis of a range of novel quinoxaline-alkynyl derivatives. It was then necessary to undertake in-vitro testing to investigate the compounds’ biological activity.

The researchers discovered that compounds with a Nitro group were especially efficacious, prompting the group to develop a hypothesis around the role of the Nitro group in the structure-activity relationship.

They discovered that the introduction of the Nitro group seemed to improve the activity of the synthesized compounds – a phenomenon that had also been observed during other studies of anti-tuberculosis agents.

For example, the recently approved anti-TB drug, Delamanid, features a Nitro group that plays a significant role in the compound’s activity.

The paper also outlines a number of quinoxaline compounds that could have the potential to act as treatments for other diseases such as malaria.

These quinoxalines had been tested against malaria and cancer, demonstrating promising anticancer results. Work is ongoing in collaboration with computational chemists in order to synthesize more derivatives of these compounds with improved activity against TB and cancer.

Gross pathology of lung tuberculosis.

Gross pathology of lung tuberculosis. Image Credit: Robert Carswell Good JM, Cooper S, Doane AS (1835). The Study of Medicine. Harper. p. 32. Archived from the original on 10 August 2016.

Asynt’s work in chemistry labs

Chemistry labs are leading the way in developing the next affordable drug for diseases such as TB and Malaria, which are particularly common in developing countries such as Africa and Asia.

Research in these spaces is rewarding, demanding and challenging, with many students contributing to projects, working on funding applications and supporting collaborative and interdisciplinary work.

Dr. Leboho’s group has been working with Asynt since 2019 and has been employing the company’s DrySyn heating blocks and waterless CondenSyn reflux condensers since that time.

The DrySyn heating block system removes the need for heating oil, which is prone to leaving a mess, while the waterless condensers allow the lab to save significant amounts of water.

The next stages of medicinal research

Drug discovery has moved away from the development of drugs to target numerous ailments, moving towards designing drugs that target specific enzymes controlling specific functions of a pathogen.

This leap has been made possible via computer-aided drug discovery, and it is anticipated that medicinal chemistry will be dominated by machine learning in the future, much like computer-aided drug discovery is currently dominating this field.

The use of biologics rather than synthetic organic compounds is also becoming more commonplace.

About Asynt

Asynt was formed in July 2003 with the aim to develop, supply and support new, sustainable and novel products central to the laboratory.

Since inception, they have developed the DrySyn range (a clean, safe alternative to oil baths and heating mantles) both reducing costs in purchasing / disposal of oil and a 35% reduction in energy consumption.

They also take pride in reducing laboratory water consumption using their air cooled CondenSyn units and highly effective water circulators.

The current team has over 70 years of experience in the scientific sector and work hard to help their customers find the best possible solutions for their requirements.

Key product lines available include Asynt ReactoMate Controlled Lab Reactors, the DrySyn heating and cooling blocks, and tools from Grant, IKA, Julabo, Huber, Porvair, Telstar and Vacuubrand amongst others. With a broad range of scientific equipment and consumables ranging from bench top laboratory scale to pilot plant and beyond both in the chemical and biological sectors.

Asynt’s Managing Director, Martyn Fordham, spent almost twenty years dealing with the requirements of research chemists (at the outset just custom glassblowing) before forming Asynt. For Martyn, having the right staff who are both knowledgeable and dedicated to customer support has been the key to Asynt’s successful growth.


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Last updated: Apr 21, 2022 at 1:12 PM

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